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Items: 1 to 20 of 102

1.

Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor.

Giordanetto F, Wållberg A, Knerr L, Selmi N, Ullah V, Thorstensson F, Lindelöf Å, Karlsson S, Nikitidis G, Llinas A, Wang QD, Lindqvist A, Högberg G, Lindhardt E, Åstrand A, Duker G.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):119-24. doi: 10.1016/j.bmcl.2012.10.140. Epub 2012 Nov 12.

PMID:
23200256
2.

Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers.

Park JE, Ji WK, Jang JW, Pae AN, Choi K, Choi KH, Kang J, Roh EJ.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1887-90. doi: 10.1016/j.bmcl.2012.12.072. Epub 2013 Jan 12.

PMID:
23395659
3.

NNC 55-0396 [(1S,2S)-2-(2-(N-[(3-benzimidazol-2-yl)propyl]-N-methylamino)ethyl)-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphtyl cyclopropanecarboxylate dihydrochloride]: a new selective inhibitor of T-type calcium channels.

Huang L, Keyser BM, Tagmose TM, Hansen JB, Taylor JT, Zhuang H, Zhang M, Ragsdale DS, Li M.

J Pharmacol Exp Ther. 2004 Apr;309(1):193-9. Epub 2004 Jan 12.

4.

Synthesis and SAR studies of a novel series of T-type calcium channel blockers.

Park SJ, Park SJ, Lee MJ, Rhim H, Kim Y, Lee JH, Chung BY, Lee JY.

Bioorg Med Chem. 2006 May 15;14(10):3502-11. Epub 2006 Jan 24.

PMID:
16434203
5.

T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.

Smith EM, Sorota S, Kim HM, McKittrick BA, Nechuta TL, Bennett C, Knutson C, Burnett DA, Kieselgof J, Tan Z, Rindgen D, Bridal T, Zhou X, Jia YP, Dong Z, Mullins D, Zhang X, Priestley T, Correll CC, Tulshian D, Czarniecki M, Greenlee WJ.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4602-6. doi: 10.1016/j.bmcl.2010.06.012. Epub 2010 Jun 8.

PMID:
20580233
6.

Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.

Shipe WD, Barrow JC, Yang ZQ, Lindsley CW, Yang FV, Schlegel KA, Shu Y, Rittle KE, Bock MG, Hartman GD, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Uebele VN, Nuss CE, Connolly TM, Doran SM, Fox SV, Kraus RL, Marino MJ, Graufelds VK, Vargas HM, Bunting PB, Hasbun-Manning M, Evans RM, Koblan KS, Renger JJ.

J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10.

PMID:
18540666
7.

Synthesis and biological evaluation of 4-piperidinecarboxylate and 4-piperidinecyanide derivatives for T-type calcium channel blockers.

Woo HM, Lee YS, Roh EJ, Seo SH, Song CM, Chung HJ, Pae AN, Shin KJ.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5910-5. doi: 10.1016/j.bmcl.2011.07.087. Epub 2011 Jul 29.

PMID:
21843937
8.

Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.

Yang ZQ, Barrow JC, Shipe WD, Schlegel KA, Shu Y, Yang FV, Lindsley CW, Rittle KE, Bock MG, Hartman GD, Uebele VN, Nuss CE, Fox SV, Kraus RL, Doran SM, Connolly TM, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Marino MJ, Graufelds VK, DiLella AG, Reynolds IJ, Vargas HM, Bunting PB, Woltmann RF, Magee MM, Koblan KS, Renger JJ.

J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26.

PMID:
18817368
9.
10.

Novel T-type calcium channel blockers: dioxoquinazoline carboxamide derivatives.

Jo MN, Seo HJ, Kim Y, Seo SH, Rhim H, Cho YS, Cha JH, Koh HY, Choo H, Pae AN.

Bioorg Med Chem. 2007 Jan 1;15(1):365-73. Epub 2006 Oct 10.

PMID:
17035033
12.

Synthesis and SAR study of T-type calcium channel blockers. Part II.

Choe YJ, Seo HN, Jung SY, Rhim H, Kim J, Choo DJ, Lee JY.

Arch Pharm (Weinheim). 2008 Oct;341(10):661-4. doi: 10.1002/ardp.200800079.

PMID:
18816587
13.

In vitro characterization of T-type calcium channel antagonist TTA-A2 and in vivo effects on arousal in mice.

Kraus RL, Li Y, Gregan Y, Gotter AL, Uebele VN, Fox SV, Doran SM, Barrow JC, Yang ZQ, Reger TS, Koblan KS, Renger JJ.

J Pharmacol Exp Ther. 2010 Nov;335(2):409-17. doi: 10.1124/jpet.110.171058. Epub 2010 Aug 3.

14.

Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers.

Campiani G, Fiorini I, De Filippis MP, Ciani SM, Garofalo A, Nacci V, Giorgi G, Sega A, Botta M, Chiarini A, Budriesi R, Bruni G, Romeo MR, Manzoni C, Mennini T.

J Med Chem. 1996 Jul 19;39(15):2922-38.

PMID:
8709127
15.

Towards selective antagonists of T-type calcium channels: design, characterization and potential applications of NNC 55-0396.

Li M, Hansen JB, Huang L, Keyser BM, Taylor JT.

Cardiovasc Drug Rev. 2005 Summer;23(2):173-96.

PMID:
16007233
16.

Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers.

Gu SJ, Lee JK, Pae AN, Chung HJ, Rhim H, Han SY, Min SJ, Cho YS.

Bioorg Med Chem Lett. 2010 May 1;20(9):2705-8. doi: 10.1016/j.bmcl.2010.03.084. Epub 2010 Mar 28.

PMID:
20382529
17.

3D pharmacophore based virtual screening of T-type calcium channel blockers.

Doddareddy MR, Choo H, Cho YS, Rhim H, Koh HY, Lee JH, Jeong SW, Pae AN.

Bioorg Med Chem. 2007 Jan 15;15(2):1091-105. Epub 2006 Oct 30.

PMID:
17074493
18.

In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.

Jang SJ, Choi HW, Choi DL, Cho S, Rim HK, Choi HE, Kim KS, Huang M, Rhim H, Lee KT, Lee JY.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6656-62. doi: 10.1016/j.bmcl.2013.10.049. Epub 2013 Oct 31.

PMID:
24220170
19.

Synthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers.

Lee HK, Lee YS, Roh EJ, Rhim H, Lee JY, Shin KJ.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4424-7. doi: 10.1016/j.bmcl.2008.06.037. Epub 2008 Jun 14.

PMID:
18625556
20.

Lead discovery and optimization of T-type calcium channel blockers.

Park JH, Choi JK, Lee E, Lee JK, Rhim H, Seo SH, Kim Y, Doddareddy MR, Pae AN, Kang J, Roh EJ.

Bioorg Med Chem. 2007 Feb 1;15(3):1409-19. Epub 2006 Nov 10.

PMID:
17150365

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